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  • 1
    Language: English
    In: Journal of Chromatography B, 2011, Vol.879(20), pp.1741-1747
    Description: Norcantharidin (NCTD), the demethylated analogue of cantharidin, inhibits the proliferation of a variety of human tumor cell lines, and appears to cause the least nephrotoxic and inflammatory side effects. Although NCTD has been used to treat human cancers in China for years, there is no report regarding its metabolism up to now. This is the first report to separate and identify the main metabolites of NCTD in vivo by GC–MS using TMS derivatives. Two hydrolyzed products and five phase I or phase II metabolites were found in rat by the chromatogram comparisons of the blank with incurred biological samples. Multiple stages of fragmentation patterns were used to confirm the metabolites characterizations. The established GC–MS method can also be applied to identifying unknown metabolites of the drugs containing hydroxyl or carbonyl groups in molecular structure.
    Keywords: Norcantharidin ; Metabolites ; Gc–MS ; Derivate ; Metabolism ; Anatomy & Physiology
    ISSN: 1570-0232
    E-ISSN: 1873-376X
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  • 2
    In: Molecular BioSystems, 2012, Vol.8(8), pp.2197-2204
    Description: Epilepsy is a cryptogenic neurological disorder characterized by recurrent seizures which may be precipitated by a variety of endogenous or exogenous factors, and usually occurs many months or years after a precipitating injury. Timely diagnosis and treatment at the early stage of epilepsy are very important for patients to prevent serious lesions and improve the quality of their life. In this study, the metabonomics approach based on the GC-MS technique, multivariate statistical analysis and the metabolism network analysis were applied to investigate metabolic changes in epileptic patients. The outcome of this study suggested that ten endogenous metabolites and five metabolism pathways were mainly involved and showed marked perturbations in epileptic patients. It not only enhances the understanding of the pathology of epilepsy, but also provides an experimental foundation for the therapeutic strategy of epilepsy. Furthermore, this work demonstrates the powerful predictive potential of the metabolic network analysis to neurological disease.
    Keywords: Epilepsy -- Blood ; Gas Chromatography-Mass Spectrometry -- Methods ; Metabolomics -- Methods;
    ISSN: 1742-206X
    E-ISSN: 1742-2051
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  • 3
    In: Biomedical Chromatography, March 2014, Vol.28(3), pp.348-353
    Description: Glucuronidation plays critical role in the elimination of bergenin; however the metabolic mechanism of UDP‐glucuronosyltransferases (UGTs) in the process remains to be investigated. In this study, the kinetics of bergenin glucuronidation by pooled human liver microsomes (HLMs) and 12 recombinat UGT isozymes were investigated. The glucuronidation of bergenin can be shown in HLMs with a value of 231.62 ± 14.08 µ and a value of 2.17 ± 0.21 nmol/min/(mg protein). Among the 12 human UGTs investigated, UGT1A1 was identified as the major isoform catalyzing the glucuronidation of bergenin [ value of 200.37 ± 26.73 µ and value of 1.88 ± 0.26 nmol/min/(mg protein)]. The bergenin glucuronosyltransferase activities in HLMs and UGT1A1 were inhibited by phenylbutazone, estradiol and bilirubin. The results demonstrate that bergenin glucuronidation in HLMs is specifically catalyzed by UGT1A1. Copyright © 2013 John Wiley & Sons, Ltd.
    Keywords: Bergenin ; Udp‐Glucuronosyltransferases ; Human Liver Microsomes ; Ugt1a1 ; In Vitro
    ISSN: 0269-3879
    E-ISSN: 1099-0801
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  • 4
    In: Journal of Bioequivalence & Bioavailability, 2013, Vol.04(07)
    ISSN: Journal of Bioequivalence & Bioavailability
    E-ISSN: 09750851
    Source: CrossRef
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  • 5
    In: Journal of Analytical Sciences, Methods and Instrumentation, 2012, Vol.02(01), pp.24-28
    Description: A new and simple gas chromatographic (GC) method using flame ionization detector (FID) and mass spectrometry (MS) for the simultaneous determination of eight fatty alcohols in 10 mg policosanol film-coated tablets was established and applied to the quality control (QC) of policosanol film-coated tablets. A DB-35MS capillary column (30 m × 0.32 mm, 0.25 um) was employed for the separation. GC-FID was used to quantitatively analyze the eight ingredients with 1-eicosanol as internal standard, three of which were identified using GC-MS due to the lack of standard. The linearity, accuracy, precision, stability, robustness and sensitivity within the detection limits were evaluated. The average recovery of the method was 96.3% - 100.4% and linearity was (R > 0.999). The average drug content was found to be 96.8% of the labeled amount (10 mg).
    Keywords: Policosanol ; Fatty Alcohols ; Gas Chromatography-Mass Spectrometry ; Gas Chromatography-Hydrogen Flame Ionization Detector;
    ISSN: 2164-2745
    E-ISSN: 2164-2753
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  • 6
    In: Fundamental & Clinical Pharmacology, October 2015, Vol.29(5), pp.478-487
    Description: Ligustrazine is the most abundant and bioactive ingredient in Rhizoma Chuanxiong, a Chinese medicinal herb commonly used for the treatment of cardiovascular diseases. Chf197 is one of the structurally modified ligustrazine derivatives in a purpose of overcoming the rapid metabolism and short half‐life of original. The plasma and urine pharmacokinetics of Chf197 in rats were studied after intravenous or intraperitoneal injection of Chf197 with the validated ‐ method. The pharmacokinetic parameters of Chf197 injected intravenously 20 mg/kg were as follows: C, 1.44 ± 0.4 mg/L; T, 0.08 h; , 3.03 ± 1.67 h; , 3.85 ± 3.88 h/L; V, 31.66 ± 11.79L/kg; and , 9.29 ± 4.92 l/h/kg. Dose‐dependent pharmacokinetics was observed, and a significantly higher dose‐normalized after intravenous administration was obtained than that after intraperitoneal administration. A possible metabolite was detected at about 3.1 min, and full‐scan mass spectrum was adopted to predict its possible structure.
    Keywords: Cardiovascular Diseases ; Chf197 ; Ligustrazine ; Metabolism ; Pharmacokinetic
    ISSN: 0767-3981
    E-ISSN: 1472-8206
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  • 7
    Language: English
    In: Biomedical Chromatography, Oct, 2012, Vol.26(10), p.1176(7)
    Description: Byline: Dujuan Zhang, Yanni Teng, Keguang Chen, Sha Liu, Chunmin Wei, Benjie Wang, Guiyan Yuan, Rui Zhang, Xiaoyan Liu, Ruichen Guo ABSTRACT A sensitive and selective liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) was developed and validated for the determination of salbutamol in human plasma and urine, and successfully applied to the pharmacokinetic study of salbutamol in Chinese healthy volunteers after inhalation of salbutamol sulfate aerosol. Salbutamol and the internal standard (IS) acetaminophen in plasma and urine were extracted with ethyl acetate, separated on a C.sub.18 reversed-phase column, eluted with mobile phase of acetonitrile-ammonium acetate (5m m; 30:70, v/v), ionized by positive ion pneumatically assisted electrospray and detected in the multi-reaction monitoring mode using precursoraproduct ions of m/z 240.2a148.1 for salbutamol and 152a110 for the IS. The lower limits of quantitation of salbutamol in human plasma and urine by this method were 0.02 and 1ng/mL, respectively. The specificity, matrix effect, recovery, sensitivity, linearity, accuracy, precision and several stabilities were validated for salbutamol in human plasma and urine. In conclusion, the validation results showed that this method is robust, specific and sensitive, and can successfully fulfill the requirement of clinical pharmacokinetic study of salbutamol in healthy Chinese volunteers. Copyright A[c] 2011 John Wiley & Sons, Ltd. Correspondence: Ruichen Guo, Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, 107 West Wenhua Road Jinan 250012, People's Republic of China. E-mail: grc7636@126.com
    Keywords: Mass Spectrometry ; Antiasthmatic Agents ; Albuterol ; Esters ; Liquid Chromatography
    ISSN: 0269-3879
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  • 8
    In: Biomedical Chromatography, November 2013, Vol.27(11), pp.1398-1405
    Description: Bergenin is the major component of and with many biological activities. Although bergenin has been used to treat human diseases in China for man years, there is no report regarding its metabolism. This is the first report to separate and identify the metabolites of bergenin . In the study, HPLC/Q‐TOF‐MS/MS was used to investigate the metabolites of bergenin by analyzing the rat body fluid and feces samples. Three metabolites of bergenin were finally identified by the TIC chromatograms, and the structures were also confirmed by their MS spectra. Copyright © 2013 John Wiley & Sons, Ltd.
    Keywords: Bergenin ; In Vivo ; Metabolites ; Hplc/Q‐Tof‐Ms/Ms
    ISSN: 0269-3879
    E-ISSN: 1099-0801
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  • 9
    In: Journal of Bioequivalence & Bioavailability, 2011, Vol.03(04)
    ISSN: Journal of Bioequivalence & Bioavailability
    E-ISSN: 09750851
    Source: CrossRef
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  • 10
    Language: English
    In: Pharmacology & Pharmacy, Oct, 2011, Vol.2(4), p.341(6)
    Keywords: Rosuvastatin -- Measurement ; Rosuvastatin -- Research ; Mass Spectrometry -- Usage ; Liquid Chromatography -- Usage
    ISSN: 2157-9423
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